2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC DNA Methyltransferase
  4. DNMT/HDAC-IN-1

DNMT/HDAC-IN-1 (Compund 15a) is a dual DNMT and HDAC inhibitor with IC50 values for HDAC1 and HDAC6 are 56.84 nM and 17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in tumor research.

For research use only. We do not sell to patients.

DNMT/HDAC-IN-1

DNMT/HDAC-IN-1 Chemical Structure

CAS No. : 2095619-17-1

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Based on 1 publication(s) in Google Scholar

DNMT/HDAC-IN-1 Related Antibodies

Top Publications Citing Use of Products

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DNA Methyltransferase DNMT1 DNMT3 MGMT

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DNMT/HDAC-IN-1 (Compund 15a) is a dual DNMT and HDAC inhibitor with IC50 values for HDAC1 and HDAC6 are 56.84 nM and 17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in tumor research.

IC50 & Target

HDAC1

56.84 nM (IC50)

HDAC6

17.39 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
K562 IC50
2.85 μM
Compound: 15a
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
[PMID: 28419930]
U-937 IC50
1.06 μM
Compound: 15a
Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
[PMID: 28419930]
In Vitro

DNMT/HDAC-IN-1 significantly suppress K562 and U937 proliferation with IC50 values of 2.85 and 1.06 mM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DNMT/HDAC-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: U937 cells
Concentration: 0, 1, 2.5, 5 μM
Incubation Time: 12 h
Result: induced histone H3K9 and histone H4K8 acetylation and increased P16 expression.

Apoptosis Analysis[1]

Cell Line: U937 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 36 h
Result: induced apoptosis in U937 cells.
In Vivo
Animal Model: female BALB/c wild-type mice[2]
Dosage: 50 mg/kg
Administration: I.v.; daily; 21 days
Result: inhibited tumor growth.
Molecular Weight

412.79

Formula

C19H16ClF3N2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NO)/C=C/C1=CC=C(C=C1)CCNC(C2=C(C=CC(C(F)(F)F)=C2)Cl)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (242.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4225 mL 12.1127 mL 24.2254 mL
5 mM 0.4845 mL 2.4225 mL 4.8451 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (6.06 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4225 mL 12.1127 mL 24.2254 mL 60.5635 mL
5 mM 0.4845 mL 2.4225 mL 4.8451 mL 12.1127 mL
10 mM 0.2423 mL 1.2113 mL 2.4225 mL 6.0563 mL
15 mM 0.1615 mL 0.8075 mL 1.6150 mL 4.0376 mL
20 mM 0.1211 mL 0.6056 mL 1.2113 mL 3.0282 mL
25 mM 0.0969 mL 0.4845 mL 0.9690 mL 2.4225 mL
30 mM 0.0808 mL 0.4038 mL 0.8075 mL 2.0188 mL
40 mM 0.0606 mL 0.3028 mL 0.6056 mL 1.5141 mL
50 mM 0.0485 mL 0.2423 mL 0.4845 mL 1.2113 mL
60 mM 0.0404 mL 0.2019 mL 0.4038 mL 1.0094 mL
80 mM 0.0303 mL 0.1514 mL 0.3028 mL 0.7570 mL
100 mM 0.0242 mL 0.1211 mL 0.2423 mL 0.6056 mL
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DNMT/HDAC-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DNMT/HDAC-IN-12095619-17-1HDACDNA MethyltransferaseHistone deacetylasesDNMTsDNA MTasesEpigenetic targetsMulti-targetAntitumor bioactivityDNMTInhibitorinhibitorinhibit

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